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CCR7 inhibitor Cmp1205

Chemical Structure : CCR7 inhibitor Cmp1205

CAS No.: 681514-83-0

CCR7 inhibitor Cmp1205 (Cmp2105)

Catalog No.: PC-73250Not For Human Use, Lab Use Only.

CCR7 inhibitor Cmp1205 is an allosteric ligand and antagonist for human CC chemokine receptor 7 (CCR7) with Kd of 3 nM, suppresses arrestin binding in response to activation by CCL19 with IC50 of 7.3 uM.

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    Biological Activity

    CCR7 inhibitor Cmp1205 is an allosteric ligand and antagonist for human CC chemokine receptor 7 (CCR7) with Kd of 3 nM, suppresses arrestin binding in response to activation by CCL19 with IC50 of 7.3 uM.
    Cmp1205 binds to a pocket at the intracellular part of CCR7 between the ends of TM1, TM2, TM3, and TM6 and the loop between TM7 and H8.
    Cmp1205 allosterically inhibits binding of the native chemokine CCL19 ligand in a membrane-based competition binding experiment with IC50 of 35 nM.

    Physicochemical Properties

    M.Wt 475.56
    Formula C22H29N5O5S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    Benzamide, 3-[[4-[[(1R)-2,2-dimethyl-1-(5-methyl-2-furanyl)propyl]amino]-1,1-dioxido-1,2,5-thiadiazol-3-yl]amino]-2-hydroxy-N,N,6-trimethyl-

    References

    1. Kathrin Jaeger, et al. Cell. 2019 Aug 22;178(5):1222-1230.e10.

    2. Proj M, et al. Front Pharmacol. 2022 Mar 18;13:855653.

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